Etifoxine hydrochloride
(Synonyms: 盐酸艾替伏辛,Stresam;HOE 36-801) 目录号 : GC15264A positive allosteric modulator of GABAA receptors
Cas No.:56776-32-0
Sample solution is provided at 25 µL, 10mM.
Etifoxine hydrochloride (HOE 36-801 hydrochlorid) is potentiator of GABAA receptor function in cultured neurons. Etifoxine preferentially acts on β2 or β3 subunit-containing GABAA receptors. IC50 value:Target: GABAA receptorEtifoxine exhibits anxiolytic activity in rodents and humans with no sedative, myorelaxant or mnesic side effects. Etifoxine acts as a ligand of the translocator protein (TSPO); promotes axonal regeneration.
References:
[1]. Verleye M, Dumas S, Heulard I, et al. Differential effects of etifoxine on anxiety-like behaviour and convulsions in BALB/cByJ and C57BL/6J mice: any relation to overexpression of central GABAA receptor beta2 subunits Eur Neuropsychopharmacol. 2011 Jun;21(6):457-70.
[2]. Bourin M, Hascot M. Implication of 5-HT2 receptor subtypes in the mechanism of action of the GABAergic compound etifoxine in the four-plate test in Swiss mice. Behav Brain Res. 2010 Apr 2;208(2):352-8.
[3]. Gee KW, Tran MB, Hogenkamp DJ, et al. Limiting activity at beta1-subunit-containing GABAA receptor subtypes reduces ataxia. J Pharmacol Exp Ther. 2010 Mar;332(3):1040-53.
[4]. Aouad M, Charlet A, Rodeau JL, et al. Reduction and prevention of vincristine-induced neuropathic pain symptoms by the non-benzodiazepine anxiolytic etifoxine are mediated by 3alpha-reduced neurosteroids. Pain. 2009 Dec 15;147(1-3):54-9.
[5]. Girard C, Liu S, Cadepond F, et al. Etifoxine improves peripheral nerve regeneration and functional recovery. Proc Natl Acad Sci U S A. 2008 Dec 23;105(51):20505-10.
Cas No. | 56776-32-0 | SDF | |
别名 | 盐酸艾替伏辛,Stresam;HOE 36-801 | ||
化学名 | 6-chloro-N-ethyl-4-methyl-4-phenyl-3,1-benzoxazin-2-amine;hydrochloride | ||
Canonical SMILES | CCNC1=NC2=C(C=C(C=C2)Cl)C(O1)(C)C3=CC=CC=C3.Cl | ||
分子式 | C17H18Cl2N2O | 分子量 | 337.24 |
溶解度 | ≥ 33.7 mg/mL in DMSO with gentle warming, ≥ 48.1 mg/mL in EtOH with gentle warming, ≥ 15.49 mg/mL in Water with gentle warming | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.9652 mL | 14.8262 mL | 29.6525 mL |
5 mM | 0.593 mL | 2.9652 mL | 5.9305 mL |
10 mM | 0.2965 mL | 1.4826 mL | 2.9652 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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